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Effect of the plant matrix on the uptake of luteolin derivatives-containing Artemisia afra aqueous-extract in Caco-2 cells.
J Ethnopharmacol. 2010 Aug 09; 130(3):439-49.JE

Abstract

AIM OF THE STUDY

Luteolin is a major flavonoid constituent and a primary candidate that might contribute to the claimed in vivo protective effects of Artemisia afra (Jacq. Ex. Willd). However, an exhaustive search yielded no literature evidence on the absorption, metabolism and fate of this flavonoid from the traditional plant preparation. The purpose of this study was to investigate the effect of the plant matrix on the uptake of luteolin derivatives from Artemisia afra aqueous extract in human intestinal epithelial Caco-2 cells.

MATERIALS AND METHODS

Cell monolayers were incubated with 5, 10 and 20 microg/ml doses of luteolin aglycone, luteolin-7-0-glucoside, un-hydrolyzed or acid-hydrolyzed Artemisia afra extracts, and samples of 150 microl each were collected from both apical and basolateral sides of cells at 30, 60 and 120 min for HPLC and LC-MS analyses.

RESULTS

After 1-h exposure, the uptake of luteolin aglycone and luteolin-7-0-glucoside from the un-hydrolyzed and acid-hydrolyzed extracts was significantly faster and quantitatively higher (i.e. >77% vs. <25% of the initial doses over the first 30 min, p<0.05) than that from non-plant solutions. Apical to basolateral permeability coefficients for luteolin and its-7-0-glucoside in the extracts were 1.6- to 2-fold higher than that for the non-plant solutions. Glucuronidation was an important pathway of metabolism for luteolin in both non-plant and plant extract forms.

CONCLUSIONS

Luteolin in Artemisia afra aqueous extract, regardless of its form (i.e. whether aglycone and 7-0-glucoside), is taken up better and more efficiently metabolized than the aglycone and 7-0-glucoside forms administered as pure solutions in Caco-2 cells. Flavonoid actives from Artemisia afra plant extracts and especially traditionally prepared dosage forms may thus have better bioavailability, and consequently greater in vivo potency, than that predicted from studies done using the pure solutions.

Links

Publisher Full Text

Authors+Show Affiliations

Mukinda JT
Discipline of Pharmacology, School of Pharmacy, University of the Western Cape, Bellville, South Africa. jamesmukind@gmail.com
Syce JA
No affiliation info available
Fisher D
No affiliation info available
Meyer M
No affiliation info available

MeSH

ArtemisiaBiological AvailabilityCaco-2 CellsCell SurvivalChromatography, High Pressure LiquidChromatography, LiquidDose-Response Relationship, DrugFlavonoidsGlucuronidesHumansIntestinal AbsorptionLuteolinMass SpectrometryPermeabilityPlant ExtractsTime Factors

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20609422

Citation

Mukinda, James T., et al. "Effect of the Plant Matrix On the Uptake of Luteolin Derivatives-containing Artemisia Afra Aqueous-extract in Caco-2 Cells." Journal of Ethnopharmacology, vol. 130, no. 3, 2010, pp. 439-49.
Mukinda JT, Syce JA, Fisher D, et al. Effect of the plant matrix on the uptake of luteolin derivatives-containing Artemisia afra aqueous-extract in Caco-2 cells. J Ethnopharmacol. 2010;130(3):439-49.
Mukinda, J. T., Syce, J. A., Fisher, D., & Meyer, M. (2010). Effect of the plant matrix on the uptake of luteolin derivatives-containing Artemisia afra aqueous-extract in Caco-2 cells. Journal of Ethnopharmacology, 130(3), 439-49. https://doi.org/10.1016/j.jep.2010.05.058
Mukinda JT, et al. Effect of the Plant Matrix On the Uptake of Luteolin Derivatives-containing Artemisia Afra Aqueous-extract in Caco-2 Cells. J Ethnopharmacol. 2010 Aug 9;130(3):439-49. PubMed PMID: 20609422.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of the plant matrix on the uptake of luteolin derivatives-containing Artemisia afra aqueous-extract in Caco-2 cells. AU - Mukinda,James T, AU - Syce,James A, AU - Fisher,David, AU - Meyer,Mervin, Y1 - 2010/06/02/ PY - 2010/04/07/received PY - 2010/05/21/revised PY - 2010/05/25/accepted PY - 2010/7/9/entrez PY - 2010/7/9/pubmed PY - 2010/11/4/medline SP - 439 EP - 49 JF - Journal of ethnopharmacology JO - J Ethnopharmacol VL - 130 IS - 3 N2 - AIM OF THE STUDY: Luteolin is a major flavonoid constituent and a primary candidate that might contribute to the claimed in vivo protective effects of Artemisia afra (Jacq. Ex. Willd). However, an exhaustive search yielded no literature evidence on the absorption, metabolism and fate of this flavonoid from the traditional plant preparation. The purpose of this study was to investigate the effect of the plant matrix on the uptake of luteolin derivatives from Artemisia afra aqueous extract in human intestinal epithelial Caco-2 cells. MATERIALS AND METHODS: Cell monolayers were incubated with 5, 10 and 20 microg/ml doses of luteolin aglycone, luteolin-7-0-glucoside, un-hydrolyzed or acid-hydrolyzed Artemisia afra extracts, and samples of 150 microl each were collected from both apical and basolateral sides of cells at 30, 60 and 120 min for HPLC and LC-MS analyses. RESULTS: After 1-h exposure, the uptake of luteolin aglycone and luteolin-7-0-glucoside from the un-hydrolyzed and acid-hydrolyzed extracts was significantly faster and quantitatively higher (i.e. >77% vs. <25% of the initial doses over the first 30 min, p<0.05) than that from non-plant solutions. Apical to basolateral permeability coefficients for luteolin and its-7-0-glucoside in the extracts were 1.6- to 2-fold higher than that for the non-plant solutions. Glucuronidation was an important pathway of metabolism for luteolin in both non-plant and plant extract forms. CONCLUSIONS: Luteolin in Artemisia afra aqueous extract, regardless of its form (i.e. whether aglycone and 7-0-glucoside), is taken up better and more efficiently metabolized than the aglycone and 7-0-glucoside forms administered as pure solutions in Caco-2 cells. Flavonoid actives from Artemisia afra plant extracts and especially traditionally prepared dosage forms may thus have better bioavailability, and consequently greater in vivo potency, than that predicted from studies done using the pure solutions. SN - 1872-7573 UR - https://www.unboundmedicine.com/medline/citation/20609422/Effect_of_the_plant_matrix_on_the_uptake_of_luteolin_derivatives_containing_Artemisia_afra_aqueous_extract_in_Caco_2_cells_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-8741(10)00378-8 DB - PRIME DP - Unbound Medicine ER -